hif 2α in 1

HIF-2α-IN-1 is a potent inhibitor of HIF-2α, with IC50 values below 500 nM.

HIF-1 2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α. Its inhibitory effect on HIF-2α activity is significant, with an IC 50 value of 0.92 μM. Furthermore, HIF-1 2α-IN-1 has the ability to decrease HIF-1α levels. This compound is particularly valuable for research on clear cell renal cell carcinoma (ccRCC) [1].

HIF-1 2α-IN-2 is a potent inhibitor of HIF-1 2α that effectively reduces HIF-1 2α levels and elicits an iron starvation response by specifically targeting ISCA2, a key protein in Iron-Sulfur Cluster Assembly 2. [1]

HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC 50 value of 6 nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer , liver disease, inflammatory disease, pulmonary diseases and iron load disorders .

This novel compound is an orally bioavailable antagonist of P2X3 P2X2 3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2 3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2 3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1 2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of less than 50 nM [1].

HIF-2α-IN-6 (117) is a HIF-2α inhibitor [1].

Selective HIF-1 dimerization inhibitor. Blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). Inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cance

HIF-2α-IN-9 (compound 35r) is an HIF-2α inhibitor that effectively suppresses VEGF-A with an IC50 of 305 nM, modulates growth-promoting genes within tumor cells, and reactivates macrophage-mediated tumor immunity [1].

CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane agent that demonstrates effectiveness in inhibiting Ras activation and the downstream effector ERK1 2 pathway, thus effectively combating pancreatic tumor formation in mice. Additionally, CMC2.24 exerts potent inhibitory effects on zinc-dependent MMPs, with IC50s ranging from 2.0-69 μM. Furthermore, CMC2.24 aids in alleviating the progression of osteoarthritis by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis through the NF-κB HIF-2α axis[1][2][3].